Structural Features for Functional Selectivity at Serotonin Receptors

Daniel Wacker1, Chong Wang1, Vsevolod Katritch1, Gye Won Han1, Xi-Ping Huang2, Eyal Vardy2, John D. McCorvy2, Yi Jiang1,3, Meihua Chu1, Fai Yiu Siu1, Wei Liu1, H. Eric Xu3,4, Vadim Cherezov1, Bryan L. Roth2,*, Raymond C. Stevens1,*

Drugs active at G protein–coupled receptors (GPCRs) can differentially modulate either canonical or noncanonical signaling pathways via a phenomenon known as functional selectivity or biased signaling. We report biochemical studies that show that the hallucinogen lysergic acid diethylamide (LSD), its precursor ergotamine (ERG), and related ergolines display strong functional selectivity for β-arrestin signaling at the 5-hydroxytryptamine (5-HT) receptor 5-HT2B, while being relatively unbiased at the 5-HT1B receptor. To investigate the structural basis for biased signaling, we determined the crystal structure of the human 5-HT2B receptor bound to ERG, and compared it with the 5-HT1B/ERG structure. Given the relatively poor understanding of GPCR structure-function to date, insight into different GPCR signaling pathways is important to better understand both adverse and favorable therapeutic activities.

• 以上资料由西亚试剂：http://www.xiyashiji.com/ 提供此产品的详细信息如密度,含量,分子式,分子量等均可在西亚官网查询   
• 相关产品如诺卡氏菌液(-)-樟脑神经鞘磷脂,从牛脑所得 杨梅苷愈创奥IAPN-叔丁基苯硫腈氯化物4-溴苯基五氟化硫色胺盐酸盐4-溴噻吩-2-甲醛纤维素粉 7-(二甲基氨基)-4-三氟甲基香豆素邻硝基苯肼盐酸盐3,3'-二氨基联苯胺四盐酸盐水合物美伐他汀丁卡因阿卡明全氟辛基季胺碘化物布西拉明硫酸多粘菌素B益母草浸膏黄苓干膏 L-2,3-二氨基丙酸盐酸盐黄糊精EB替代品(GoldView)等均有销售.欢迎订购